Fungal infections affect most of the people sometime or other in life and create major problems in treatment of immunocompromised patients and those suffering from AIDS. The total number of these types of patients is increasing in recent years and it has become the need of the hour to have effective antifungal agents. The current antifungal agents belong to various groups like polyenes, allylamines, azoles, glucan synthesis inhibitors etc. Fluconazole is an important member of the family of azole antifungals as it is orally active and has low toxicity but its extensive use has resulted in emergence of fluconazole-resistant fungal strains. It is therefore necessary to develop analogues of fluconazole effective against resistant strains. Worldwide efforts to obtain fluconazole analogues effective against resistant strains have resulted in synthesis of many novel azole antifungals but the synthesis of ideal antifungal agent is yet to be achieved.
The structure-activity relationship studies have shown that presence of one triazole ring, halogenated phenyl ring and tertiary alcoholic oxygen functionality in fluconazole is necessary for its activity. The present invention seeks to provide novel azoles and process thereof as an effort to come up with antifungal agents with broad spectrum of antifungal activity. Fluconazole analogues have been reported to exhibit antifungal activity in the literature. Some of the references describing synthesis and antifungal activity of fluconazole analogues are:
Chemistry and Biodiversity 4, 1472-9 (2007); Bioorg Med Chem Lett 17 (13), 3686-9 (2007); J Med Chem 48 (6), 2184-93 (2005); Phosphorus Sulfur and Silicon 179, 2329-34 (2004).
The compounds described in the present invention are novel compounds with enhanced antifungal activity and hence the protection is sought for the same.